WO2004062609A3 - Derives de pyrimidine utilises comme antagonistes des recepteurs de l'il-8 - Google Patents

Derives de pyrimidine utilises comme antagonistes des recepteurs de l'il-8 Download PDF

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Publication number
WO2004062609A3
WO2004062609A3 PCT/US2004/000584 US2004000584W WO2004062609A3 WO 2004062609 A3 WO2004062609 A3 WO 2004062609A3 US 2004000584 W US2004000584 W US 2004000584W WO 2004062609 A3 WO2004062609 A3 WO 2004062609A3
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WO
WIPO (PCT)
Prior art keywords
alkyl
receptor antagonists
pyrimidine derivatives
compounds
formula
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Application number
PCT/US2004/000584
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English (en)
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WO2004062609A2 (fr
Inventor
Shawn David Erickson
John J Baldwin
Ronald E Dolle Iii
James Inglese
Michael H J Ohlmeyer
Koc-Kan Ho
Adolph C Bohnstedt
Steven G Kultgen
Maria L Webb
Douglas S Auld
Andrew Laird Roughton
Paolo Giovanni Martino C Conti
Dirk Leysen
Der Louw Jaap Van
Original Assignee
Pharmacopeia Inc
Shawn David Erickson
John J Baldwin
Ronald E Dolle Iii
James Inglese
Michael H J Ohlmeyer
Koc-Kan Ho
Adolph C Bohnstedt
Steven G Kultgen
Maria L Webb
Douglas S Auld
Andrew Laird Roughton
Paolo Giovanni Martino C Conti
Dirk Leysen
Der Louw Jaap Van
Akzo Nobel Nv
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Application filed by Pharmacopeia Inc, Shawn David Erickson, John J Baldwin, Ronald E Dolle Iii, James Inglese, Michael H J Ohlmeyer, Koc-Kan Ho, Adolph C Bohnstedt, Steven G Kultgen, Maria L Webb, Douglas S Auld, Andrew Laird Roughton, Paolo Giovanni Martino C Conti, Dirk Leysen, Der Louw Jaap Van, Akzo Nobel Nv filed Critical Pharmacopeia Inc
Publication of WO2004062609A2 publication Critical patent/WO2004062609A2/fr
Publication of WO2004062609A3 publication Critical patent/WO2004062609A3/fr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/42One nitrogen atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne des composés contenant un noyau pyrimidine ainsi que leur utilisation pour traiter des maladies et des états pathologiques associés à une activité inappropriée des récepteurs de l'interleukine 8. Ces composés sont représentés par la formule (I). Dans lesdits composés, Q est de préférence hétérocyclyle non substitué et substitué, U est normalement hydrogène ou fluor, et V est de préférence hydrogène, halogène, alkyle, -O-alkyle ou S-alkyle. La formule (X) constitue un exemple représentatif.
PCT/US2004/000584 2003-01-10 2004-01-09 Derives de pyrimidine utilises comme antagonistes des recepteurs de l'il-8 WO2004062609A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US10/340,398 2003-01-10
US10/340,398 US7037916B2 (en) 1999-07-15 2003-01-10 Pyrimidine derivatives as IL-8 receptor antagonists

Publications (2)

Publication Number Publication Date
WO2004062609A2 WO2004062609A2 (fr) 2004-07-29
WO2004062609A3 true WO2004062609A3 (fr) 2004-11-25

Family

ID=32711323

Family Applications (1)

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PCT/US2004/000584 WO2004062609A2 (fr) 2003-01-10 2004-01-09 Derives de pyrimidine utilises comme antagonistes des recepteurs de l'il-8

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US (1) US7037916B2 (fr)
WO (1) WO2004062609A2 (fr)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2008228768A1 (en) * 2007-03-22 2008-09-25 Vertex Pharmaceuticals Incorporated N-heterocyclic compounds useful as inhibitors of Janus Kinases
DE102010000662A1 (de) 2009-03-18 2010-10-21 Bayer Cropscience Ag Aminopropylthiazol-Derivate als Fungizide
BR112014016147B8 (pt) * 2011-12-30 2022-10-11 Dow Agrosciences Llc Pirimidinas-2,6-dialo-5-alcóxi-4-substituídas, pirimidina-carbaldeídos, e seus métods de formação e uso
IN2014DN07636A (fr) 2012-03-16 2015-05-15 Vitae Pharmaceuticals Inc
RS55532B1 (sr) 2012-03-16 2017-05-31 Vitae Pharmaceuticals Inc Modulatori jetrenog x receptora
CN103374005B (zh) * 2012-04-11 2016-12-14 南京信诺泰医药有限公司 取代呋喃并哌啶衍生物的合成新方法
EP2988742A4 (fr) * 2013-04-22 2016-10-19 Abbvie Inc Thiazoles et utilisations de ceux-ci
US9359336B2 (en) 2014-10-09 2016-06-07 Allergan, Inc. Heterocycle-substituted pyridyl benzothiophenes as kinase inhibitors
CN109890364B (zh) * 2016-10-03 2023-10-17 儿童医疗中心公司 糖尿病肾病的预防和治疗

Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0826673A1 (fr) * 1995-04-13 1998-03-04 Dainippon Pharmaceutical Co., Ltd. Derives de l'acetamide, procede de fabrication et composition medicamenteuse a base de ces derives
JPH10130150A (ja) * 1996-09-05 1998-05-19 Dainippon Pharmaceut Co Ltd 酢酸アミド誘導体からなる医薬
WO1998037079A1 (fr) * 1997-02-19 1998-08-27 Berlex Laboratories, Inc. Derives n-heterocycliques utiles en tant qu'inhibiteurs de la no synthetase
WO2001005783A1 (fr) * 1999-07-15 2001-01-25 Pharmacopeia, Inc. Antagonistes du recepteur b1 de la bradykinine
EP1110951A1 (fr) * 1998-08-27 2001-06-27 Sumitomo Pharmaceuticals Company, Limited Derives de pyrimidine
WO2003002542A1 (fr) * 2000-12-22 2003-01-09 Bristol-Myers Squibb Company Inhibiteurs n-heterocycliques de l'expression de tnf-alpha
WO2003077656A1 (fr) * 2002-03-15 2003-09-25 Ciba Specialty Chemicals Holding Inc. 4-aminopyrimidines et leur utilisation pour le traitement antimicrobien de surfaces
WO2004018435A1 (fr) * 2002-08-24 2004-03-04 Astrazeneca Ab Derives de la pyrimidine utilises comme modulateurs d'activite du recepteur de chimiokine
WO2004063192A1 (fr) * 2003-01-10 2004-07-29 Pharmacopeia Drug Discovery, Inc. Derives de d'imidazolyl pyrimidine utilises comme modulateurs du recepteur de il-8
WO2004069829A1 (fr) * 2003-01-10 2004-08-19 Pharmacopeia Drug Discovery, Inc. Derives d'aminoethylamide d'acide (2s)-2-((pyrimidin-4-yl)amino)-4-methylpentanoique utilises comme modulateurs du recepteur de l'il-8 pour traiter l'atherosclerose et la polyarthrite rhumatoide

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JPS6339875A (ja) 1986-08-05 1988-02-20 Nissin Food Prod Co Ltd ピリミジン誘導体
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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0826673A1 (fr) * 1995-04-13 1998-03-04 Dainippon Pharmaceutical Co., Ltd. Derives de l'acetamide, procede de fabrication et composition medicamenteuse a base de ces derives
JPH10130150A (ja) * 1996-09-05 1998-05-19 Dainippon Pharmaceut Co Ltd 酢酸アミド誘導体からなる医薬
WO1998037079A1 (fr) * 1997-02-19 1998-08-27 Berlex Laboratories, Inc. Derives n-heterocycliques utiles en tant qu'inhibiteurs de la no synthetase
EP1110951A1 (fr) * 1998-08-27 2001-06-27 Sumitomo Pharmaceuticals Company, Limited Derives de pyrimidine
WO2001005783A1 (fr) * 1999-07-15 2001-01-25 Pharmacopeia, Inc. Antagonistes du recepteur b1 de la bradykinine
WO2003002542A1 (fr) * 2000-12-22 2003-01-09 Bristol-Myers Squibb Company Inhibiteurs n-heterocycliques de l'expression de tnf-alpha
WO2003077656A1 (fr) * 2002-03-15 2003-09-25 Ciba Specialty Chemicals Holding Inc. 4-aminopyrimidines et leur utilisation pour le traitement antimicrobien de surfaces
WO2004018435A1 (fr) * 2002-08-24 2004-03-04 Astrazeneca Ab Derives de la pyrimidine utilises comme modulateurs d'activite du recepteur de chimiokine
WO2004063192A1 (fr) * 2003-01-10 2004-07-29 Pharmacopeia Drug Discovery, Inc. Derives de d'imidazolyl pyrimidine utilises comme modulateurs du recepteur de il-8
WO2004069829A1 (fr) * 2003-01-10 2004-08-19 Pharmacopeia Drug Discovery, Inc. Derives d'aminoethylamide d'acide (2s)-2-((pyrimidin-4-yl)amino)-4-methylpentanoique utilises comme modulateurs du recepteur de l'il-8 pour traiter l'atherosclerose et la polyarthrite rhumatoide

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Title
E. F. ELSLAGER ET AL.: "Synthesis and Antimalarial Effects of 1-(3,4-Dichlorophenyl)-3-[4-[(1-ethyl-3-piperidyl)amino]-6-methyl-2-pyrimidinyl]guanidine and Related Substances", J. MED. CHEM., vol. 17, no. 1, 1974, pages 75 - 100, XP002297230 *
PATENT ABSTRACTS OF JAPAN vol. 1998, no. 10 31 August 1998 (1998-08-31) *

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US20040087601A1 (en) 2004-05-06
US7037916B2 (en) 2006-05-02
WO2004062609A2 (fr) 2004-07-29

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